- Topical & Transdermal Therapies
- Benefits of Transdermal NSAIDs
- Topical Anesthetics
- Iontophoresis & Phonophoresis
- Pregame Rubs
- Hemorrhoids
- Excessive Perspiration
- Transdermal Medications
- Examples of Compounded Medications
Topical Peripheral tissue activity
Systemic side effects less likely
If analgesic, applied directly over painful site
Insignificant serum levels
Transdermal Systemic activity Potential for adverse effects If analgesic, may be applied away from painful site Serum levels necessary for effect
Medications that relieve pain, reduce inflammation, and relax muscles can have side effects that are detrimental to athletic performance, such as drowsiness. However, when these medications are administered topically, the therapeutic benefit can be enhanced while significantly reducing the risk of adverse effects.
For example, research has shown that topically-applied ketoprofen provides a high local concentration of drug below the site of application but decreases systemic exposure and significantly reduces the risk of gastrointestinal upset or bleeding. When properly compounded into an appropriate base, tissue concentrations of ketoprofen were found to be 100-fold greater below the application site (knee) compared to systemic concentrations. Muscle relaxants can be similarly prepared to minimize the risk of drowsiness.
A symposium held during the 93rd Annual Congress of the Italian Society of Orthopedics and Traumatology (SIOT) in Rome, Italy in November 2008, noted that topical anti-inflammatory therapy is a promising therapeutic strategy in the treatment of muscle strains, since it provides local analgesic and anti-inflammatory effects while minimizing systemic adverse events.
Adv Ther. 2009 Dec;26(12):1072-83. Epub 2010 Feb 4. New therapeutic approaches for management of sport-induced muscle strains. De Carli A et al. Click here to access the PubMed abstract of this article.
Transdermal Systemic activity Potential for adverse effects If analgesic, may be applied away from painful site Serum levels necessary for effect
Medications that relieve pain, reduce inflammation, and relax muscles can have side effects that are detrimental to athletic performance, such as drowsiness. However, when these medications are administered topically, the therapeutic benefit can be enhanced while significantly reducing the risk of adverse effects.
For example, research has shown that topically-applied ketoprofen provides a high local concentration of drug below the site of application but decreases systemic exposure and significantly reduces the risk of gastrointestinal upset or bleeding. When properly compounded into an appropriate base, tissue concentrations of ketoprofen were found to be 100-fold greater below the application site (knee) compared to systemic concentrations. Muscle relaxants can be similarly prepared to minimize the risk of drowsiness.
A symposium held during the 93rd Annual Congress of the Italian Society of Orthopedics and Traumatology (SIOT) in Rome, Italy in November 2008, noted that topical anti-inflammatory therapy is a promising therapeutic strategy in the treatment of muscle strains, since it provides local analgesic and anti-inflammatory effects while minimizing systemic adverse events.
Adv Ther. 2009 Dec;26(12):1072-83. Epub 2010 Feb 4. New therapeutic approaches for management of sport-induced muscle strains. De Carli A et al. Click here to access the PubMed abstract of this article.
To avoid the risks of COX-2 inhibitors, our pharmacy can compound topically applied NSAIDs such as ibuprofen and ketoprofen. Topical NSAIDs have a safety profile which is superior to oral formulations. Topical NSAID administration offers the advantage of local, enhanced delivery to painful sites with a reduced incidence of systemic adverse effects.
Topical preparations can be customized to contain a combination of medications to meet the specific needs of each patient.
Topical NSAIDs for Acute Pain “Topical non-steroidal anti-inflammatory drugs have a lower incidence of gastrointestinal adverse effects than the same drugs when they are taken orally. The low incidence of systemic adverse effects for topical NSAIDs probably results from the much lower plasma concentration from similar doses applied topically to those administered orally. Topical application of ibuprofen resulted in measurable tissue concentrations in deep tissue compartments, more than enough to inhibit inflammatory enzymes.” Topical NSAIDs have not been associated with renal failure.
BMJ. 1995 Jul 1;311(6996):22-6 Topical non-steroidal anti-inflammatory drugs and admission to hospital for upper gastrointestinal bleeding and perforation: a record linkage case-control study. Free full text article available at bmj.com: http://bmj.bmjjournals.com/cgi/content/full/311/6996/22
QJM 1995;88:551–557 Non-steroidal anti-inflammatory drugs and hospitalization for acute renal failure. Click here to access the PubMed abstract of this article.
The following article concludes: “Topical non-steroidal anti-inflammatory drugs are effective in relieving pain in acute and chronic conditions.”
BMJ. 1998 Jan 31;316(7128):333-8 Quantitative systematic review of topically applied non-steroidal anti-inflammatory drugs. Click here to access the PubMed abstract of this article. Free full text article available at bmj.com: http://bmj.bmjjournals.com/cgi/content/full/316/7128/333
The following article reports “The systemic concentrations of ketoprofen have also been found to be 100 fold lower compared to tissue concentrations below the application site in patients undergoing knee joint surgery. Topically applied ketoprofen thus provides high local concentration below the site of application but lower systemic exposure.”
Pharm Res. 1996 Jan;13(1):168-72 Percutaneous absorption of ketoprofen from different anatomical sites in man. Click here to access the PubMed abstract of this article.
Findings of this study demonstrate that "following topical application in a patch, ketoprofen shows rapid and sustained delivery to the underlying tissues without a significant increase of the plasma drug concentration."
AAPS PharmSciTech. 2010 Mar;11(1):154-8. Epub 2010 Jan 20. Ketoprofen absorption by muscle and tendon after topical or oral administration in patients undergoing anterior cruciate ligament reconstruction. Sekiya I, Mo.rito T, Hara K, Yamazaki J, Ju YJ, Yagishita K, Mochizuki T, Tsuji K, Muneta T. Click here to access the PubMed abstract of this article.
Reduction of spontaneous pain and pain on active movement in the topical ketoprofen spray group was significantly greater than in the oral ketoprofen treatment group, irrespective of sprain severity. Regarding mobility impairment and ankle swelling, topically-applied ketoprofen treatment turned out to be significantly superior to orally administered ketoprofen treatment. Additionally, the topical preparation was well tolerated, whereas ketoprofen tablets caused gastrointestinal side effects in some patients.
Minerva Cardioangiol. 2008 Oct;56(5 Suppl):47-53. Management of uncomplicated ankle sprains with topical or oral ketoprofen treatment. A registry study. Vinciguerra G et al. Click here to access the PubMed abstract of this article.
Topical NSAIDs have a safety profile which is superior to oral formulations. Topical NSAID administration offers the advantage of local, enhanced delivery to painful sites with higher tissue levels beneath the site of application and a reduced incidence of systemic (such as gastrointestinal) adverse effects.
Advanced Studies in Medicine, Johns Hopkins University, Volume 3 (7A), July 2003
This study concluded that topical NSAIDs, when used for treatment of pain resulting from strains, sprains or sports or overuse-type injuries, can provide good levels of pain relief without the systemic adverse events associated with oral NSAIDs.
Cochrane Database Syst Rev. 2010 Jun 16; 6: CD007402. Topical NSAIDs for acute pain in adults. Massey T, Derry S, Moore RA, McQuay HJ. Click here to access the PubMed abstract of this article.
Topical preparations can be customized to contain a combination of medications to meet the specific needs of each patient.
Topical NSAIDs for Acute Pain “Topical non-steroidal anti-inflammatory drugs have a lower incidence of gastrointestinal adverse effects than the same drugs when they are taken orally. The low incidence of systemic adverse effects for topical NSAIDs probably results from the much lower plasma concentration from similar doses applied topically to those administered orally. Topical application of ibuprofen resulted in measurable tissue concentrations in deep tissue compartments, more than enough to inhibit inflammatory enzymes.” Topical NSAIDs have not been associated with renal failure.
BMJ. 1995 Jul 1;311(6996):22-6 Topical non-steroidal anti-inflammatory drugs and admission to hospital for upper gastrointestinal bleeding and perforation: a record linkage case-control study. Free full text article available at bmj.com: http://bmj.bmjjournals.com/cgi/content/full/311/6996/22
QJM 1995;88:551–557 Non-steroidal anti-inflammatory drugs and hospitalization for acute renal failure. Click here to access the PubMed abstract of this article.
The following article concludes: “Topical non-steroidal anti-inflammatory drugs are effective in relieving pain in acute and chronic conditions.”
BMJ. 1998 Jan 31;316(7128):333-8 Quantitative systematic review of topically applied non-steroidal anti-inflammatory drugs. Click here to access the PubMed abstract of this article. Free full text article available at bmj.com: http://bmj.bmjjournals.com/cgi/content/full/316/7128/333
The following article reports “The systemic concentrations of ketoprofen have also been found to be 100 fold lower compared to tissue concentrations below the application site in patients undergoing knee joint surgery. Topically applied ketoprofen thus provides high local concentration below the site of application but lower systemic exposure.”
Pharm Res. 1996 Jan;13(1):168-72 Percutaneous absorption of ketoprofen from different anatomical sites in man. Click here to access the PubMed abstract of this article.
Findings of this study demonstrate that "following topical application in a patch, ketoprofen shows rapid and sustained delivery to the underlying tissues without a significant increase of the plasma drug concentration."
AAPS PharmSciTech. 2010 Mar;11(1):154-8. Epub 2010 Jan 20. Ketoprofen absorption by muscle and tendon after topical or oral administration in patients undergoing anterior cruciate ligament reconstruction. Sekiya I, Mo.rito T, Hara K, Yamazaki J, Ju YJ, Yagishita K, Mochizuki T, Tsuji K, Muneta T. Click here to access the PubMed abstract of this article.
Reduction of spontaneous pain and pain on active movement in the topical ketoprofen spray group was significantly greater than in the oral ketoprofen treatment group, irrespective of sprain severity. Regarding mobility impairment and ankle swelling, topically-applied ketoprofen treatment turned out to be significantly superior to orally administered ketoprofen treatment. Additionally, the topical preparation was well tolerated, whereas ketoprofen tablets caused gastrointestinal side effects in some patients.
Minerva Cardioangiol. 2008 Oct;56(5 Suppl):47-53. Management of uncomplicated ankle sprains with topical or oral ketoprofen treatment. A registry study. Vinciguerra G et al. Click here to access the PubMed abstract of this article.
Topical NSAIDs have a safety profile which is superior to oral formulations. Topical NSAID administration offers the advantage of local, enhanced delivery to painful sites with higher tissue levels beneath the site of application and a reduced incidence of systemic (such as gastrointestinal) adverse effects.
Advanced Studies in Medicine, Johns Hopkins University, Volume 3 (7A), July 2003
This study concluded that topical NSAIDs, when used for treatment of pain resulting from strains, sprains or sports or overuse-type injuries, can provide good levels of pain relief without the systemic adverse events associated with oral NSAIDs.
Cochrane Database Syst Rev. 2010 Jun 16; 6: CD007402. Topical NSAIDs for acute pain in adults. Massey T, Derry S, Moore RA, McQuay HJ. Click here to access the PubMed abstract of this article.
Analgesic gels and sprays can be compounded to reduce pain and bleeding secondary to lacerations. The search for a "topical anesthetic that affords painless, safe application, does not contain narcotics or controlled substances, and has a maximum safety with complete anesthesia" revealed that LAT gel (lidocaine, adrenaline, tetracaine) is superior to preparations containing cocaine for topical anesthesia in laceration repair. Epinephrine (adrenaline) in the gel helps to stop bleeding secondary to injury.
Pediatrics 1995 Feb;95(2):255-8 Lidocaine adrenaline tetracaine gel versus tetracaine adrenaline cocaine gel for topical anesthesia in linear scalp and facial lacerations in children aged 5 to 17 years. Click here to access the PubMed abstract of this article.
Pediatrics 1995 Feb;95(2):255-8 Lidocaine adrenaline tetracaine gel versus tetracaine adrenaline cocaine gel for topical anesthesia in linear scalp and facial lacerations in children aged 5 to 17 years. Click here to access the PubMed abstract of this article.
Iontophoresis and phonophoresis are technologies that are capable of enhancing drug penetration through the skin. Phonophoresis uses ultrasonic waves to transmit molecules of drug through the skin, as opposed to iontophoresis, which uses low level electric current. Both techniques are used to treat inflammatory conditions such as arthritis, plantar fasciitis, tendonitis, bursitis, and carpal tunnel syndrome.
Iontophoresis of ionized drugs provided a 20-60 fold increase in penetration over topical application. Examples of successful applications of iontophoresis include:
Acetic acid iontophoresis is effective in the treatment of heel pain. Iontophoresis of dexamethasone for plantar fasciitis should be considered when more immediate results are needed. Iontophoresis has also been used to successfully treat plantar hyperhidrosis.
Phonophoresis (or sonophoresis) combines ultrasound with topical drug therapy to achieve therapeutic drug concentrations at target sites below the skin. A cream or gel containing medications such as corticosteroids, local anesthetics, electrolytes, or antibiotics is applied to the treatment area and then massaged with a transducer head. The technique has been widely used in sports medicine since the 1960s by podiatrists, orthopedists, and physical therapists.
The method of preparation and quality of ingredients used for solutions or gels for iontophoresis or phonophoresis are critical to the success of the therapy and minimizing side effects. J Am Podiatr Med Assoc. 1999 May;89(5):251-7 Management of heel pain syndrome with acetic acid iontophoresis. Click here to access the PubMed abstract of this article. Am J Sports Med. 1997 May-Jun;25(3):312-6 Treatment of plantar fasciitis by iontophoresis of 0.4% dexamethasone. A randomized, double-blind, placebo-controlled study. Click here to access the PubMed abstract of this article.
Iontophoresis of ionized drugs provided a 20-60 fold increase in penetration over topical application. Examples of successful applications of iontophoresis include:
- treatment of inflammation/pain of muscles and tendons, including the Achilles tendon
- rapid, noninvasive local anesthesia, particularly for children
- relief of heel pain from bone spurs
- controlling the pain of tennis elbow
- relief of pain from rheumatoid arthritis of the knee
- relief of pain associated with plantar fasciitis
- an alternative to steroid injections for therapy of Carpal Tunnel Syndrome
- treatment for scar and tendon adhesions
Acetic acid iontophoresis is effective in the treatment of heel pain. Iontophoresis of dexamethasone for plantar fasciitis should be considered when more immediate results are needed. Iontophoresis has also been used to successfully treat plantar hyperhidrosis.
Phonophoresis (or sonophoresis) combines ultrasound with topical drug therapy to achieve therapeutic drug concentrations at target sites below the skin. A cream or gel containing medications such as corticosteroids, local anesthetics, electrolytes, or antibiotics is applied to the treatment area and then massaged with a transducer head. The technique has been widely used in sports medicine since the 1960s by podiatrists, orthopedists, and physical therapists.
The method of preparation and quality of ingredients used for solutions or gels for iontophoresis or phonophoresis are critical to the success of the therapy and minimizing side effects. J Am Podiatr Med Assoc. 1999 May;89(5):251-7 Management of heel pain syndrome with acetic acid iontophoresis. Click here to access the PubMed abstract of this article. Am J Sports Med. 1997 May-Jun;25(3):312-6 Treatment of plantar fasciitis by iontophoresis of 0.4% dexamethasone. A randomized, double-blind, placebo-controlled study. Click here to access the PubMed abstract of this article.
Pregame rubs can be compounded to contain substances such as emu oil and anti-spasmodic drugs. Emu oil is a moisturizer that can improve healing of injured skin.
Plast Reconstr Surg 1998 Dec;102(7):2404-7 Promotion of second intention wound healing by emu oil lotion: comparative results with furasin, polysporin, and cortisone. Click here to access the PubMed abstract of this article.
Plast Reconstr Surg 1998 Dec;102(7):2404-7 Promotion of second intention wound healing by emu oil lotion: comparative results with furasin, polysporin, and cortisone. Click here to access the PubMed abstract of this article.
Hemorrhoids are particularly problematic for catchers, coaches, and others who are regularly in a squatting position. Treatment often involves use of a novel dosage form known as the "rectal rocket", a suppository that permits simultaneous internal and external application of anti-inflammatories, anesthetics, antibiotics, or other medications.
Hyperhidrosis therapy Excessive perspiration is a concern for many athletes, as well as members of dance teams and marching bands. Numerous topical treatment options exist.
Primary hyperhidrosis (excessive perspiration) is a physically and emotionally distressing condition which involves mainly the palms, soles, and axillae. Oral anticholinergic agents and beta-blockers may be effective for controlling or reducing profuse sweating, but also carry significant side effects. Topical therapies may be the most practical and most common treatment for hyperhidrosis, but many agents that have proven useful in clinical trials are not commercially available.
Placebo-controlled trials have shown that topically applied 20% aluminum chloride hexahydrate significantly reduces the symptoms of hyperhidrosis in 60%-100% of patients. Skin irritation can be minimized with 1% hydrocortisone cream or by compounding 20% aluminum chloride in a 4% salicylic acid gel base, instead of in anhydrous alcohol base (as is the commercial product Drysol®).
Luh and Blackwell of the Dept. of Internal Medicine, University of Texas Medical Branch at Galveston describe a healthy, active 27-year-old male resident physician who had excessive facial sweating with minimal exertion or stress. The sweating was especially pronounced on the forehead, nose, and upper lip. Daily topical application of a 0.5% glycopyrrolate solution to the face and forehead significantly reduced facial sweating after the first treatment, without any discomfort to the skin. No loss of efficacy was seen after multiple face washings. Facial hyperhidrosis recurred after withdrawal of the glycopyrrolate for 2 days, confirming its therapeutic effect. Two years later, he continues to use glycopyrrolate as needed.
Mayo Clin Proc 1986 Dec;61(12):951-6 Treatment of primary hyperhidrosis. Click here to access the PubMed abstract of this article.
South Med J 2002 Jul;95(7):756-8 Craniofacial hyperhidrosis successfully treated with topical glycopyrrolate. Click here to access the PubMed abstract of this article.
Ann Pharmacother 1995 May;29(5):489-92 Propantheline bromide in the management of hyperhidrosis associated with spinal cord injury. Click here to access the PubMed abstract of this article.
Intl J Pharm Comp 2001 Jan/Feb;5(1):28-9 Glycopyrrolate 1% Cream Click here to access the abstract of this article.
Primary hyperhidrosis (excessive perspiration) is a physically and emotionally distressing condition which involves mainly the palms, soles, and axillae. Oral anticholinergic agents and beta-blockers may be effective for controlling or reducing profuse sweating, but also carry significant side effects. Topical therapies may be the most practical and most common treatment for hyperhidrosis, but many agents that have proven useful in clinical trials are not commercially available.
Placebo-controlled trials have shown that topically applied 20% aluminum chloride hexahydrate significantly reduces the symptoms of hyperhidrosis in 60%-100% of patients. Skin irritation can be minimized with 1% hydrocortisone cream or by compounding 20% aluminum chloride in a 4% salicylic acid gel base, instead of in anhydrous alcohol base (as is the commercial product Drysol®).
Luh and Blackwell of the Dept. of Internal Medicine, University of Texas Medical Branch at Galveston describe a healthy, active 27-year-old male resident physician who had excessive facial sweating with minimal exertion or stress. The sweating was especially pronounced on the forehead, nose, and upper lip. Daily topical application of a 0.5% glycopyrrolate solution to the face and forehead significantly reduced facial sweating after the first treatment, without any discomfort to the skin. No loss of efficacy was seen after multiple face washings. Facial hyperhidrosis recurred after withdrawal of the glycopyrrolate for 2 days, confirming its therapeutic effect. Two years later, he continues to use glycopyrrolate as needed.
Mayo Clin Proc 1986 Dec;61(12):951-6 Treatment of primary hyperhidrosis. Click here to access the PubMed abstract of this article.
South Med J 2002 Jul;95(7):756-8 Craniofacial hyperhidrosis successfully treated with topical glycopyrrolate. Click here to access the PubMed abstract of this article.
Ann Pharmacother 1995 May;29(5):489-92 Propantheline bromide in the management of hyperhidrosis associated with spinal cord injury. Click here to access the PubMed abstract of this article.
Intl J Pharm Comp 2001 Jan/Feb;5(1):28-9 Glycopyrrolate 1% Cream Click here to access the abstract of this article.
Transdermal therapy to decrease side effects
Medications that relieve pain, reduce inflammation, and relax muscles can have side effects that are detrimental to athletic performance, such as drowsiness. However, when these medications are administered transdermally, the therapeutic benefit can be enhanced while significantly reducing the risk of adverse effects.
For example, research has shown that topically applied ketoprofen provides a high local concentration of drug below the site of application but decreases systemic exposure and significantly reduces the risk of gastrointestinal upset or bleeding. When properly compounded into an appropriate base, tissue concentrations of ketoprofen were found to be 100-fold greater below the application site (knee) compared to systemic concentrations. Muscle relaxants can be similarly prepared to minimize the risk of drowsiness. A symposium held during the 93rd Annual Congress of the Italian Society of Orthopedics and Traumatology (SIOT) in Rome, Italy in November 2008, noted that topical anti-inflammatory therapy is a promising therapeutic strategy in the treatment of muscle strains, since it provides local analgesic and anti-inflammatory effects while minimizing systemic adverse events.
Adv Ther. 2009 Dec;26(12):1072-83. Epub 2010 Feb 4. New therapeutic approaches for management of sport-induced muscle strains. De Carli A et al. Click here to access the PubMed abstract of this article.
Medications that relieve pain, reduce inflammation, and relax muscles can have side effects that are detrimental to athletic performance, such as drowsiness. However, when these medications are administered transdermally, the therapeutic benefit can be enhanced while significantly reducing the risk of adverse effects.
For example, research has shown that topically applied ketoprofen provides a high local concentration of drug below the site of application but decreases systemic exposure and significantly reduces the risk of gastrointestinal upset or bleeding. When properly compounded into an appropriate base, tissue concentrations of ketoprofen were found to be 100-fold greater below the application site (knee) compared to systemic concentrations. Muscle relaxants can be similarly prepared to minimize the risk of drowsiness. A symposium held during the 93rd Annual Congress of the Italian Society of Orthopedics and Traumatology (SIOT) in Rome, Italy in November 2008, noted that topical anti-inflammatory therapy is a promising therapeutic strategy in the treatment of muscle strains, since it provides local analgesic and anti-inflammatory effects while minimizing systemic adverse events.
Adv Ther. 2009 Dec;26(12):1072-83. Epub 2010 Feb 4. New therapeutic approaches for management of sport-induced muscle strains. De Carli A et al. Click here to access the PubMed abstract of this article.
The following list is just a few of the preparations that we can compound for sports medicine. All formulations are customized to meet the unique needs of each individual; therefore, we can consider the athlete’s lifestyle and environmental factors when formulating medications. Our compounding professionals can choose the best base to administer the active ingredients, or consult with the prescriber to determine the most appropriate route of administration to solve a specific problem.
- Clotrimazole in DMSO solution
- Cyclobenzaprine/Ketoprofen transdermal gel
- Dexamethasone iontophoresis solution
- Fluconazole/Ibuprofen topical gel
- Ketamine/Gabapentin transdermal gel
- Ketoprofen 10% transdermal gel
- LAT topical gel
- Lidocaine/Hydrocortisone "rectal rocket" suppository
- Nutritional Supplements
- Rehydration Drinks